CN105142641A - 用于治疗癌症的化合物 - Google Patents

用于治疗癌症的化合物 Download PDF

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Publication number
CN105142641A
CN105142641A CN201480013734.1A CN201480013734A CN105142641A CN 105142641 A CN105142641 A CN 105142641A CN 201480013734 A CN201480013734 A CN 201480013734A CN 105142641 A CN105142641 A CN 105142641A
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Prior art keywords
methylpyridin
amine
methyl
pyridin
quinazolin
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Pending
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CN201480013734.1A
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Chinese (zh)
Inventor
安松柱
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Curegenix Inc
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Curegenix Inc
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Publication of CN105142641A publication Critical patent/CN105142641A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
CN201480013734.1A 2013-03-12 2014-03-12 用于治疗癌症的化合物 Pending CN105142641A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361777427P 2013-03-12 2013-03-12
US61/777,427 2013-03-12
PCT/US2014/024885 WO2014165232A1 (fr) 2013-03-12 2014-03-12 Composés pour le traitement du cancer

Publications (1)

Publication Number Publication Date
CN105142641A true CN105142641A (zh) 2015-12-09

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CN201480013734.1A Pending CN105142641A (zh) 2013-03-12 2014-03-12 用于治疗癌症的化合物

Country Status (8)

Country Link
US (3) US9713612B2 (fr)
EP (1) EP2968348A4 (fr)
JP (1) JP2016518328A (fr)
KR (1) KR20150125665A (fr)
CN (1) CN105142641A (fr)
AU (1) AU2014248568B2 (fr)
CA (1) CA2905830C (fr)
WO (1) WO2014165232A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105348298A (zh) * 2014-07-04 2016-02-24 沈阳中化农药化工研发有限公司 取代芳基吡啶类化合物及其用途
WO2017167150A1 (fr) * 2016-03-31 2017-10-05 苏州云轩医药科技有限公司 Composé hétérocyclique 3-fluoropyridine et son application
CN108685923A (zh) * 2018-06-07 2018-10-23 广州源生医药科技有限公司 Wnt信号通路抑制剂在治疗LGR5阳性癌症中的应用
CN110506129A (zh) * 2016-12-21 2019-11-26 新加坡科技研究局 用于鉴定恶性肿瘤的试剂盒及其用途
CN110678466A (zh) * 2017-03-30 2020-01-10 豪夫迈·罗氏有限公司 作为hpk1抑制剂的二氮杂萘类
CN114072408A (zh) * 2019-07-08 2022-02-18 南京明德新药研发有限公司 作为porcupine抑制剂的化合物及其应用

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SG11201408237YA (en) * 2012-06-15 2015-01-29 Curegenix Inc Compound as wnt signaling inhibitor, composition, and use thereof
AU2013289990B2 (en) 2012-07-13 2018-06-14 Oncomed Pharmaceuticals, Inc. RSPO3 binding agents and uses thereof
CA2905830C (fr) 2013-03-12 2022-01-18 Curegenix Inc. Derives de quinazoline et de naphtyridine utiles dans le traitement du cancer
CA2961374A1 (fr) 2014-09-16 2016-03-24 Oncomed Pharmaceuticals, Inc. Traitement de maladies fibrotiques
MA41123A (fr) * 2014-12-02 2017-10-10 Oncomed Pharm Inc Polythérapie pour le traitement du cancer
CN107708699A (zh) * 2015-05-26 2018-02-16 源生公司 肿瘤生物标志物及其应用
CA2985818A1 (fr) * 2015-05-31 2016-12-08 Curegenix Corporation Compositions de combinaison comprenant un antagoniste de porcupine et un antagoniste de l'axe pd-l/pd-1 aux fins d'immunotherapie
GB201516504D0 (en) 2015-09-17 2015-11-04 Astrazeneca Ab Imadazo(4,5-c)quinolin-2-one Compounds and their use in treating cancer
WO2017062688A1 (fr) * 2015-10-08 2017-04-13 Suzhou Yunxuan Yiyao Keji Youxian Gongsi Inhibiteurs de la voie de signalisation wnt et leurs applications thérapeutiques
KR102698411B1 (ko) * 2015-10-08 2024-08-26 쑤저우 운씨엔 이야오 커지 요씨엔 공시 Wnt 신호 전달 경로 억제제 및 이의 치료적 적용
CN105254613A (zh) * 2015-10-08 2016-01-20 苏州云轩医药科技有限公司 具有Wnt信号通路抑制活性的杂环化合物及其应用
WO2017095918A2 (fr) * 2015-12-01 2017-06-08 Oncomed Pharmaceuticals, Inc. Procédés de traitement du cancer au moyen d'antagonistes de rspo3
WO2017162611A1 (fr) * 2016-03-21 2017-09-28 Astrazeneca Ab Composés quinoline-3-carboxamide et leur utilisation pour traiter le cancer
KR102476709B1 (ko) 2016-11-21 2022-12-09 나노스트링 테크놀로지스, 인크. 화학적 조성물 및 이것을 사용하는 방법
CN107441045B (zh) 2017-07-21 2018-10-19 广州源生医药科技有限公司 用于递送Wnt信号通路抑制剂的脂质体制剂及其制备方法
CA3072362A1 (fr) 2017-10-06 2019-04-11 Forma Therapeutics, Inc. Inhibition de la peptidase 30 specifique de l'ubiquitine
AU2019271028A1 (en) 2018-05-14 2020-12-03 Bruker Spatial Biology, Inc. Chemical compositions and methods of using same
BR112020021921A2 (pt) 2018-05-17 2021-01-26 Forma Therapeutics, Inc. compostos bicíclicos fundidos úteis como inibidores de peptidase 30 específica de ubiquitina
US10961534B2 (en) 2018-07-13 2021-03-30 University of Pittsburgh—of the Commonwealth System of Higher Education Methods of treating porphyria
LT3860989T (lt) 2018-10-05 2023-06-12 Forma Therapeutics, Inc. Sulieti pirolinai, kurie veikia kaip ubikvitinui specifinės proteazės 30 (ups30) inhibitoriai

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SG11201408237YA (en) 2012-06-15 2015-01-29 Curegenix Inc Compound as wnt signaling inhibitor, composition, and use thereof
CA2905830C (fr) 2013-03-12 2022-01-18 Curegenix Inc. Derives de quinazoline et de naphtyridine utiles dans le traitement du cancer
CN107708699A (zh) 2015-05-26 2018-02-16 源生公司 肿瘤生物标志物及其应用

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105348298A (zh) * 2014-07-04 2016-02-24 沈阳中化农药化工研发有限公司 取代芳基吡啶类化合物及其用途
CN105348298B (zh) * 2014-07-04 2019-03-19 沈阳中化农药化工研发有限公司 取代芳基吡啶类化合物及其用途
WO2017167150A1 (fr) * 2016-03-31 2017-10-05 苏州云轩医药科技有限公司 Composé hétérocyclique 3-fluoropyridine et son application
CN110506129A (zh) * 2016-12-21 2019-11-26 新加坡科技研究局 用于鉴定恶性肿瘤的试剂盒及其用途
CN110506129B (zh) * 2016-12-21 2023-06-30 新加坡科技研究局 用于鉴定恶性肿瘤的试剂盒及其用途
CN110678466A (zh) * 2017-03-30 2020-01-10 豪夫迈·罗氏有限公司 作为hpk1抑制剂的二氮杂萘类
CN110678466B (zh) * 2017-03-30 2023-01-31 豪夫迈·罗氏有限公司 作为hpk1抑制剂的二氮杂萘类
CN108685923A (zh) * 2018-06-07 2018-10-23 广州源生医药科技有限公司 Wnt信号通路抑制剂在治疗LGR5阳性癌症中的应用
CN114072408A (zh) * 2019-07-08 2022-02-18 南京明德新药研发有限公司 作为porcupine抑制剂的化合物及其应用
CN114072408B (zh) * 2019-07-08 2023-05-12 南京明德新药研发有限公司 作为porcupine抑制剂的化合物及其应用

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KR20150125665A (ko) 2015-11-09
JP2016518328A (ja) 2016-06-23
US10660889B2 (en) 2020-05-26
US9713612B2 (en) 2017-07-25
EP2968348A4 (fr) 2016-11-09
CA2905830A1 (fr) 2014-10-09
US20170304302A1 (en) 2017-10-26
WO2014165232A1 (fr) 2014-10-09
CA2905830C (fr) 2022-01-18
AU2014248568A1 (en) 2015-09-17
EP2968348A1 (fr) 2016-01-20
US20160000780A1 (en) 2016-01-07
US10238652B2 (en) 2019-03-26
AU2014248568B2 (en) 2017-07-13
US20190142827A1 (en) 2019-05-16

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